2. Apoptosis Metabolic Enzyme/Protease
  3. Glutathione Peroxidase Ferroptosis
  4. GPX4-IN-5

GPX4-IN-5 is a covalent inhibitor of GPX4 (IC50: 0.12 μM). GPX4-IN-5 can induce ferroptosis and has anti-tumor effects. GPX4-IN-5 can be used in the study of triple-negative breast cancer (TNBC).

For research use only. We do not sell to patients.

GPX4-IN-5

GPX4-IN-5 Chemical Structure

CAS No. : 2922824-09-5

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Based on 1 publication(s) in Google Scholar

GPX4-IN-5 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GPX4-IN-5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GPX4-IN-5 is a covalent inhibitor of GPX4 (IC50: 0.12 μM). GPX4-IN-5 can induce ferroptosis and has anti-tumor effects. GPX4-IN-5 can be used in the study of triple-negative breast cancer (TNBC)[1].

IC50 & Target

IC50: 0.12 μM (GPX4)[1]
In Vitro

GPX4-IN-5 (Compound 18) (72 hours) has antitumor activity against TNBC cells (MDA-MB-468, BT-549, MDA-MB-468) with IC50s of 0.01, 0.075, and 0.012 μM, respectively.
GPX4-IN-5 (1 μM, 72 hours) is unable to effectively kill MDA-MB-231 cells induced by ferroptosis inhibitors (Ferrostatin-1 (HY-100579), Acetylcysteine (HY-B0215), L-Glutathione reduced (HY-D0187)), indicating that it relies on ferroptosis to exert its potent cell-killing effect[1].
GPX4-IN-5 (5-20 nM, 8 hours) increases Fe2+ and ROS levels in MDA-MB-231 cells, leading to LPOs accumulation and inducing ferroptosis[1].
GPX4-IN-5 (20 nM, 6 hours) causes mitochondrial volume reduction, cristae disappearance, and outer membrane rupture in MDA-MB-231 cells, which are consistent with the characteristics of ferroptosis[1].
GPX4-IN-5 (1 hour) has significant inhibitory activity against GPX4 (IC50: 0.12 μM)[1].
GPX4-IN-5 (1 μM, 2 hours) decreases the degradation temperature of GPX4 in MDA-MB-231 cells as determined by Celular Thermal shift Assay, indicating that it can directly bind to GPX4[1].
GPX4-IN-5 (50-800 nM, 90 minutes) has a strong covalent bond formation ability with GPX4 (Kinact/KI: 93.54 min/M)[1].
GPX4-IN-5 (20 nM) slightly increases LPO in MDA-MB-231 cells transfected with siGPX4#1, and the levels of GPX4-related proteins does not change significantly, indicating that it induces cell ferroptosis by specifically targeting GPX4 protein[1].
GPX4-IN-5 (5-20 nM, 10 hours) inhibits GPX4 activity rather than downregulating GPX4 levels to induce ferroptosis in MDA-MB-231 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GPX4-IN-5 Related Antibodies

Western Blot Analysis

Cell Line: MDA-MB-231 cells
Concentration: 5, 10, 20 nM
Incubation Time: 4, 6 8, 10 h
Result: Showed a decrease in the expression levels of negative regulatory proteins of ferroptosis (GPX4 and FTH1), and the decrease in FTH1 was associated with abnormal iron metabolism.
Showed that the expression level of the xCT system was not downregulated, indicating that it was not inhibited.
Caused a compensatory upregulation of GPX4 expression within 6 hours, and then decreased after 8 hours.
Parmacokinetics[1]
Species Dose Route Indicator value
Rat 10 mg/kg i.p. T1/2 1.90 hr
Rat 10 mg/kg i.p. Tmax 0.85 hr
Rat 10 mg/kg i.p. Cmax 5205 ng/mL
Rat 10 mg/kg i.p. AUC0-t 12.099 ng·h/mL
Rat 10 mg/kg i.p. MRT0-t 1.71 hr
Rat 10 mg/kg i.p. CL 0.83 L/h/kg
In Vivo

GPX4-IN-5 (Compound 18) (5-20 mg/kg, i.p., once a day for 21 consecutive days) has significant anti-tumor activity in the MDA-MB-231 xenograft tumor BALB/C nude mouse model, and has no obvious damage to kidney, liver and heart function[1].
GPX4-IN-5 (20 mg/kg, i.p., once a day for 14 consecutive days) has no obvious blood toxicity, does not cause bone marrow suppression, and has no obvious damage to kidney, liver and heart function in the BALB/C nude mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (female, aged 4 weeks) injected with MDA-MB-231 (8 million cells)[1]
Dosage: 5, 10, 20 mg/kg
Administration: i.p. once a day, 21 consecutive days
Result: Showed excellent tumor growth inhibition (TGI) ranging from 50.4% to 81.0%.
Showed no obvious drug-related damage in organs such as heart, liver, spleen, lung and kidney.
Can significantly reduce the level of GPX4 protein in tumor tissues, indicating that it can effectively induce ferroptosis in vivo.
Reduced the number of Ki67-positive tumor cells and inhibited the proliferation of tumor cells.
Animal Model: BALB/c nude mice (female, aged 4 weeks)[1]
Dosage: 20 mg/kg
Administration: i.p. once a day, 14 consecutive days
Result: Showed no significant differences in ALT, AST, BUN, CREA, LDH, and CK, indicated that the kidney, liver, and heart functions of the mice were not significantly damaged.
Has no obvious blood toxicity and did not cause bone marrow suppression, which is manifested by no significant changes in white blood cells (WBC), red blood cells (RBC) and hemoglobin (HGB).
Molecular Weight

381.78

Formula

C18H17ClFNO5
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

COC1=CC(N(C2=CC3=C(OCCO3)C=C2)C(CCl)=O)=CC(OC)=C1F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (261.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6193 mL 13.0965 mL 26.1931 mL
5 mM 0.5239 mL 2.6193 mL 5.2386 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.90%

SDS (251 KB)

COA (255 KB) HNMR (258 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6193 mL 13.0965 mL 26.1931 mL 65.4827 mL
5 mM 0.5239 mL 2.6193 mL 5.2386 mL 13.0965 mL
10 mM 0.2619 mL 1.3097 mL 2.6193 mL 6.5483 mL
15 mM 0.1746 mL 0.8731 mL 1.7462 mL 4.3655 mL
20 mM 0.1310 mL 0.6548 mL 1.3097 mL 3.2741 mL
25 mM 0.1048 mL 0.5239 mL 1.0477 mL 2.6193 mL
30 mM 0.0873 mL 0.4366 mL 0.8731 mL 2.1828 mL
40 mM 0.0655 mL 0.3274 mL 0.6548 mL 1.6371 mL
50 mM 0.0524 mL 0.2619 mL 0.5239 mL 1.3097 mL
60 mM 0.0437 mL 0.2183 mL 0.4366 mL 1.0914 mL
80 mM 0.0327 mL 0.1637 mL 0.3274 mL 0.8185 mL
100 mM 0.0262 mL 0.1310 mL 0.2619 mL 0.6548 mL
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GPX4-IN-5 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GPX4-IN-52922824-09-5Glutathione PeroxidaseFerroptosisTNBCGPX4MDA-MB-231cellsTNBC cellsBALB/C miceInhibitorinhibitorinhibit

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